中文名：吡非尼酮
英文名：Pirfenidone (S-7701)
英文別名：AMR-69;2(1H)-Pyridinone, 5-methyl-1-phenyl-
純度：10mM in DMSO
貨號：P409216
包裝：1ml
Cas號：53179-13-8
存儲溫度：-80℃儲存
產(chǎn)品介紹：
Information
Pirfenidone (S-7701, AMR-69) is an inhibitor forTGF-βproduction and TGF-β stimulated collagen production, reduces production ofTNF-αand IL-1β, and also has anti-fibrotic and anti-inflammatory properties. Pirfenidone attenuateschemokine (CC motif) ligand-2
In?vitro
Pirfenidone (< 300 μg/mL) suppresses the proinflammatory cytokine tumor necrosis factor-α (TNF-α) by a translational mechanism in RAW264.7 cells, which is independent of activation of the mitogen-activated protain kinase (MAPK) 2, p38 MAP kinase, and c-Jun N-terminal kinase (JNK). Pirfenidone (< 10 mM) leads to reduced glioma cell density in concentration-dependent manner in LN-18, T98G, LNT-229 and LN-308 cell lines. Pirfenidone (< 5 mM) reduces TGF-β bioactivity by affecting TGF-β2 mRNA expression and processing of pro-TGF-β in CCL-64 cells. Pirfenidone (< 8.3 mM) inhibits the activity of recombinant furin and downregulates the expression of MMP-11 in a dose-dependent manner in LN-308 cells.
In?vivo
Pirfenidone (250 mg/kg) potently inhibits the production of the proinflammatory cytokines, TNF-alpha, interferon-gamma, and interleukin-6, but enhances the production of the anti-inflammatory cytokine, interleukin-10, in mice. Pirfenidone (250 mg/kg/day) ameliorates cyclosporine-induced fibrosis by about 50% and decreases TGF-beta1 protein expression by 80% in Sprague-Dawley rats receiving a low-salt diet. Pirfenidone (400 mg/kg/day) inhibits heat shock protein 47-positive cells and myofibroblasts, the principal cells responsible for the accumulation and deposition of extracellular matrix seen in pulmonary fibrosis in ICR mice intravenously injected with bleomycin. Pirfenidone (0.5%, liquid diet) treatment reduces the degree of liver injury in rats, as determined by alanine aminotransferase values and necro-inflammatory score, which is associated with reduced hepatic stellate cells proliferation and collagen deposition. Pirfenidone (0.5%, liquid diet) administration downregulates dimethylnitrosamine induced transcripts levels of procollagen alpha1(I), TIMP-1 and MMP-2 by 50-60% in rats, and this is associated with a 70% reduction in collagen deposition.
Cell?Data
cell?lines：Melanoma cells
Concentrations：
Incubation?Time：
Powder?Purity:≥99%
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關鍵字： AMR-69;2(1H)-Pyridinone, 5-methyl-1-phenyl-
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